Oral pediatric trimethobenzamide formulations and methods

Abstract

Oral pediatric trimethobenzamide compositions and methods for treating and controlling nausea and/or vomiting are disclosed in warm blooded animals, especially humans including children. The oral pediatric trimethobenzamide compositions and methods of the present invention are believed to be at least as effective as a 200 mg intramuscular (I.M.) trimethobenzamide HCl injectable formulation when administered at a dose of about 100 mg. In addition, an oral pediatric composition containing about 120 mg of trimethobenzamide HCl is believed to be uniquely approximately bioequivalent to a 200 mg intramuscular (I.M.) trimethobenzamide HCl injectable formulation when administered at a dose of about 100 mg.

We claim:  
     
         1 ) An oral pediatric trimethobenzamide composition for treating and controlling nausea and/or vomiting in a child comprising 
 trimethobenzamide and a suitable pharmaceutical excipient, wherein said oral pediatric trimethobenzamide composition is at least about as effective as a 200 mg intramuscular (I.M.) trimethobenzamide HCl injectable formulation when administered in a dose of about 100 mg to treat and control nausea and/or vomiting.    
     
     
         2 ) An oral pediatric trimethobenzamide composition of  claim 1 , wherein said trimethobenzamide is present in an amount greater than 120 mg.  
     
     
         3 ) an oral pediatric trimethobenzamide composition of  claim 2 , wherein said trimethobenzamide is present in an amount selected from the group consisting of about 125 mg, 130 mg, 140 mg, 150 mg, 160 mg, 175, mg, 180 mg and 200 mg:  
     
     
         4 ) An oral pediatric trimethobenzamide composition of  claim 1 , wherein said trimethobenzamide is trimethobenzamide hydrochloride.  
     
     
         5 ) An oral pediatric trimethobenzamide composition of  claim 1 , wherein mean PK parameters for said oral pediatric trimethobenzamide composition are greater than mean PK parameters for the 200 mg intramuscular (I.M.) trimethobenzamide HCl injectable formulation formulation when administered in a dose of about 100 mg.  
     
     
         6 ) An oral pediatric trimethobenzamide composition of  claim 1 , wherein said oral pediatric trimethobenzamide composition is produced by the process of 
 granulating the trimethobenzamide, and    blending said pharmaceutical excipient with the granulated trimethobenzamide.    
     
     
         7 ) An oral pediatric trimethobenzamide composition of  claim 1 , wherein said oral pediatric trimethobenzamide composition is produced by the process of 
 mixing the trimethobenzamide with said pharmaceutical excipient.    
     
     
         8 ) An oral pediatric trimethobenzamide composition of  claim 1 , wherein said oral pediatric trimethobenzamide composition contains more than one pharmaceutical excipient.  
     
     
         9 ) An oral pediatric trimethobenzamide composition of  claim 8 , wherein said pediatric pharmaceutical excipients are starch, lactose and magnesium stearate.  
     
     
         10 ) An oral pediatric trimethobenzamide composition for treating and controlling nausea and/or vomiting in a child comprising 
 trimethobenzamide and a suitable pharmaceutical excipient, wherein said oral trimethobenzamide composition is approximately bioequivalent to a 200 mg intramuscular (I.M.) trimethobenzamide HCl injectable formulation when administered in a dose of about 100 mg to treat and control nausea and/or vomiting.    
     
     
         11 ) An oral pediatric trimethobenzamide composition of  claim 10 , wherein said trimethobenzamide is present in an amount of about 120 mg.  
     
     
         12 ) An oral pediatric trimethobenzamide composition of  claim 10 , wherein said trimethobenzamide is trimethobenzamide hydrochloride.  
     
     
         13 ) An oral pediatric trimethobenzamide composition of  claim 10 , wherein mean PK parameters for said composition are approximately equivalent to mean PK parameters for the 200 mg intramuscular (I.M.) trimethobenzamide HCl injectable formulation when administered in a dose of about 100 mg.  
     
     
         14 ) An oral pediatric trimethobenzamide composition of  claim 10 , wherein said oral pediatric trimethobenzamide composition is produced by the process of 
 granulating the trimethobenzamide, and    blending said pharmaceutical excipient with the granulated trimethobenzamide.    
     
     
         15 ) An oral pediatric trimethobenzamide composition of  claim 10 , wherein said oral pediatric trimethobenzamide composition is produced by the process of 
 mixing the trimethobenzamide with said pharmaceutical excipient.    
     
     
         16 ) An oral pediatric trimethobenzamide composition of  claim 10 , wherein said oral pediatric trimethobenzamide composition contains more than one pharmaceutical excipient.  
     
     
         17 ) An oral pediatric trimethobenzamide composition of  claim 16 , wherein said pharmaceutical excipients are starch, lactose and magnesium stearate.  
     
     
         18  ) An oral pediatric trimethobenzamide composition for treating and controlling nausea and/or vomiting in a child, said composition comprising 
 trimethobenzamide, and  
 a pharmaceutically acceptable excipient, wherein said oral trimethobenzamide composition, following oral administration to a warm-blooded animal, achieves plasma (exposure) levels which are at least approximately equal to or greater than those plasma (exposure) levels achieved by a FDA-approved 200 mg intramuscular (I.M.) trimethobenzamide HCl injectable formulation when administered intramuscularly to a warm-blooded animal at a dose of about 100 mg.  
 
     
     
         18 ) An oral pediatric trimethobenzamide composition of  claim 1 , wherein said trimethobenzamide is present in an amount of about 120 mg.  
     
     
         19 ) An oral pediatric trimethobenzamide composition of  claim 10 , wherein said trimethobenzamide is present in an amount greater than about 120 mg.